The chemical objectives of this research include the further development of some new organocopper reagents which introduce, in a single step, an acrylate or acrolein unit. Emphasis will be placed on the regiospecific and stereospecific construction of latent bis-alkylating agents which derive their genesis from the alpha-methylene lactone cytotoxic molecules. Through the utilization of the 2-carboxy and 2-carbaldehyde allyl systems, we hope to prepare some unique site-specific antitumor agents by combining known drugs with biological carriers which should affect tissue distributions of the drugs. The types of compounds which we propose offer new possibilities in the area of latent alkylating agents which may be enzymatically activated or modified in vivo. As the various target molecules are prepared in gram quantities, they will be sent to Dr. H.B. Wood, Jr. at N.C.I. for testing in the mouse leukemia L1210 system.